Pharmaceutical Salts and Co-crystals
Pharmaceutical Salts and Co-crystals

Author: Johan Wouters

Publisher: Royal Society of Chemistry

Published: 2011-11-04

Total Pages: 407

ISBN-13: 1849733503

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From crystal structure prediction to totally empirical screening, the quest for new crystal forms has become one of the most challenging issues in the solid state science and particularly in the pharmaceutical world. In this context, multi-component crystalline materials like co-crystals have received renewed interest as they offer the prospect of optimized physical properties. As illustrated in this first book_ entirely dedicated to this emerging class of pharmaceutical compounds_ the outcome of such endeavours into crystal engineering have demonstrated clear impacts on production, marketing and intellectual property protection of active pharmaceutical ingredients (APIs). Indeed, co-crystallization influences relevant physico-chemical parameters (such as solubility, dissolution rate, chemical stability, melting point, hygroscopicity, à) and often offers solids with properties superior to those of the free drug. Combining both reports of the latest research and comprehensive overviews of basic principles, with contributions from selected experts in both academia and industry, this unique book is an essential reference, ideal for pharmaceutical development scientists and graduate students in pharmaceutical science.

Pharmaceutical Crystals (Volume II)
Pharmaceutical Crystals (Volume II)

Author: Etsuo Yonemochi

Publisher: Mdpi AG

Published: 2023-02-07

Total Pages: 0

ISBN-13: 9783036554730

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The crystalline state is the most commonly used as an essential solid in active pharmaceutical ingredients (API). The characterization of pharmaceutical crystals encompasses many scientific disciplines. Still, the core is crystal structure analysis, which reveals the molecular structure of essential pharmaceutical compounds. Crystal structure analysis provides important structural information related to the API's wide range of physicochemical properties, such as solubility, stability, tablet performance, color, and hygroscopicity. These properties should be understood in terms of molecular structures and interactions between molecules in crystals. Information on three-dimensional molecular structures also affords insights into the biological activity of molecules. The second reprint in the series, "Crystalline Pharmaceuticals (Volume II)" focused on the relationship between crystal structure and physicochemical properties. In particular, the new crystal structure of pharmaceutical compounds involving multi-component crystals, such as co-crystals, salts and hydrates, and polymorph crystals, were reported with interest. Such crystal structures contributed to the latest studies that combine morphology, spectroscopic, theoretical calculation, and thermal analysis with the crystallographic study. Thus, this reprint highlights the importance of crystal structure information in many areas of pharmaceutical science and presents current trends in the structure-property study of pharmaceutical crystals. The Guest Editors of this reprint hope the readers enjoy a wide variety of recent studies on "Crystalline Pharmaceuticals."

Pharmaceutical Crystals
Pharmaceutical Crystals

Author: Tong Li

Publisher: John Wiley & Sons

Published: 2018-09-03

Total Pages: 578

ISBN-13: 1119046343

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An important resource that puts the focus on understanding and handling of organic crystals in drug development Since a majority of pharmaceutical solid-state materials are organic crystals, their handling and processing are critical aspects of drug development. Pharmaceutical Crystals: Science and Engineering offers an introduction to and thorough coverage of organic crystals, and explores the essential role they play in drug development and manufacturing. Written contributions from leading researchers and practitioners in the field, this vital resource provides the fundamental knowledge and explains the connection between pharmaceutically relevant properties and the structure of a crystal. Comprehensive in scope, the text covers a range of topics including: crystallization, molecular interactions, polymorphism, analytical methods, processing, and chemical stability. The authors clearly show how to find solutions for pharmaceutical form selection and crystallization processes. Designed to be an accessible guide, this book represents a valuable resource for improving the drug development process of small drug molecules. This important text: Includes the most important aspects of solid-state organic chemistry and its role in drug development Offers solutions for pharmaceutical form selection and crystallization processes Contains a balance between the scientific fundamental and pharmaceutical applications Presents coverage of crystallography, molecular interactions, polymorphism, analytical methods, processing, and chemical stability Written for both practicing pharmaceutical scientists, engineers, and senior undergraduate and graduate students studying pharmaceutical solid-state materials, Pharmaceutical Crystals: Science and Engineering is a reference and textbook for understanding, producing, analyzing, and designing organic crystals which is an imperative skill to master for anyone working in the field.

Pharmaceutical Crystals
Pharmaceutical Crystals

Author: Etsuo Yonemochi

Publisher: MDPI

Published: 2020-04-03

Total Pages: 148

ISBN-13: 3039287125

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The crystalline state is the most commonly used essential solid active pharmaceutical ingredient (API). The characterization of pharmaceutical crystals encompasses many scientific disciplines, but the core is crystal structure analysis, which reveals the molecular structure of essential pharmaceutical compounds. Crystal structure analysis provides important structural information related to the API's wide range of physicochemical properties, such as solubility, stability, tablet performance, color, and hygroscopicity. This book entitled “Pharmaceutical Crystals" focuses on the relationship between crystal structure and physicochemical properties. In particular, the new crystal structure of pharmaceutical compounds involving multi-component crystals, such as co-crystals, salts, and hydrates, and polymorph crystals are reported. Such crystal structures were investigated in the latest studies that combined morphology, spectroscopic, theoretical calculation, and thermal analysis with crystallographic study. This book highlights the importance of crystal structure information in many areas of pharmaceutical science and presents current trends in the structure–property study of pharmaceutical crystals. The Guest Editors of this book hope the readers enjoy a wide variety of recent studies on Pharmaceutical Crystals.

Pharmaceutical Crystallography
Pharmaceutical Crystallography

Author: Andrew Bond

Publisher: Royal Society of Chemistry

Published: 2019-07-24

Total Pages: 304

ISBN-13: 1788018516

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The pharmaceutical industry has become acutely aware of the importance of the solid state, but pharmaceutical scientists often lack specific training in topics related to solid-state structure and crystallography. This book provides needed support in this topical area. Taking an intuitive and informal approach to solid-state structure and crystallographic concepts, this book is written for anyone who needs a clear understanding of modern crystallography, with specific reference to small-molecule pharmaceutical solids. The author describes molecular crystals and crystal structures, symmetry, space groups, single-crystal and powder X-ray diffraction techniques and the analysis and interpretation of crystallographic data. Useful technical details are presented where necessary and case studies from the pharmaceutical literature put theory into a practical context. Written by an internationally leading figure and with its focus on molecular crystals, this book is equally applicable to chemists with a need to understand and apply X-ray crystal-structure determination.

Pharmaceutical Crystals
Pharmaceutical Crystals

Author: Tong Li

Publisher: John Wiley & Sons

Published: 2018-10-16

Total Pages: 432

ISBN-13: 1119046297

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An important resource that puts the focus on understanding and handling of organic crystals in drug development Since a majority of pharmaceutical solid-state materials are organic crystals, their handling and processing are critical aspects of drug development. Pharmaceutical Crystals: Science and Engineering offers an introduction to and thorough coverage of organic crystals, and explores the essential role they play in drug development and manufacturing. Written contributions from leading researchers and practitioners in the field, this vital resource provides the fundamental knowledge and explains the connection between pharmaceutically relevant properties and the structure of a crystal. Comprehensive in scope, the text covers a range of topics including: crystallization, molecular interactions, polymorphism, analytical methods, processing, and chemical stability. The authors clearly show how to find solutions for pharmaceutical form selection and crystallization processes. Designed to be an accessible guide, this book represents a valuable resource for improving the drug development process of small drug molecules. This important text: Includes the most important aspects of solid-state organic chemistry and its role in drug development Offers solutions for pharmaceutical form selection and crystallization processes Contains a balance between the scientific fundamental and pharmaceutical applications Presents coverage of crystallography, molecular interactions, polymorphism, analytical methods, processing, and chemical stability Written for both practicing pharmaceutical scientists, engineers, and senior undergraduate and graduate students studying pharmaceutical solid-state materials, Pharmaceutical Crystals: Science and Engineering is a reference and textbook for understanding, producing, analyzing, and designing organic crystals which is an imperative skill to master for anyone working in the field.

Polymorphism in the Pharmaceutical Industry
Polymorphism in the Pharmaceutical Industry

Author: Rolf Hilfiker

Publisher: John Wiley & Sons

Published: 2019-01-04

Total Pages: 645

ISBN-13: 3527697853

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"Polymorphism in the Pharmaceutical Industry - Solid Form and Drug Development" highlights the relevance of polymorphism in modern pharmaceutical chemistry, with a focus on quality by design (QbD) concepts. It covers all important issues by way of case studies, ranging from properties and crystallization, via thermodynamics, analytics and theoretical modelling right up to patent issues. As such, the book underscores the importance of solid-state chemistry within chemical and pharmaceutical development. It emphasizes why solid-state issues are important, the approaches needed to avoid problems and the opportunities offered by solid-state properties. The authors include true polymorphs as well as solvates and hydrates, while providing information on physicochemical properties, crystallization thermodynamics, quantum-mechanical modelling, and up-scaling. Important analytical tools to characterize solid-state forms and to quantify mixtures are summarized, and case studies on solid-state development processes in industry are also provided. Written by acknowledged experts in the field, this is a high-quality reference for researchers, project managers and quality assurance managers in pharmaceutical, agrochemical and fine chemical companies as well as for academics and newcomers to organic solid-state chemistry.

Multi-Component Crystals
Multi-Component Crystals

Author: Edward Tiekink

Publisher: Walter de Gruyter GmbH & Co KG

Published: 2017-11-20

Total Pages: 364

ISBN-13: 3110464950

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In this volume, contributions covering the theoretical and practical aspects of multicomponent crystals provide a timely and contemporary overview of the state-of-the art of this vital aspect of crystal engineering/materials science. With a solid foundation in fundamentals, multi-component crystals can be formed, for example, to enhance pharmaceutical properties of drugs, for the specific control of optical responses to external stimuli and to assemble molecules to allow chemical reactions that are generally intractable following conventional methods. Contents Pharmaceutical co-crystals: crystal engineering and applications Pharmaceutical multi-component crystals: improving the efficacy of anti-tuberculous agents Qualitative and quantitative crystal engineering of multi-functional co-crystals Control of photochromism in N-salicylideneaniline by crystal engineering Quinoline derivatives for multi-component crystals: principles and applications N-oxides in multi-component crystals and in bottom-up synthesis and applications Multi-component crystals and non-ambient conditions Co-crystals for solid-state reactivity and thermal expansion Solution co-crystallisation and its applications The salt-co-crystal continuum in halogen-bonded systems Large horizontal displacements of benzene-benzene stacking interactions in co-crystals Simultaneous halogen and hydrogen bonding to carbonyl and thiocarbonylfunctionality Crystal chemistry of the isomeric N,N’-bis(pyridin-n-ylmethyl)-ethanediamides, n = 2, 3 or 4 Solute・solvent interactions mediated by main group element (lone-pair)・・・π(aryl) interactions

Supramolecular Synthons in Crystal Engineering of Pharmaceutical Properties
Supramolecular Synthons in Crystal Engineering of Pharmaceutical Properties

Author: Ashwini K. Nangia

Publisher: CRC Press

Published: 2024-10-14

Total Pages: 199

ISBN-13: 1040124658

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This comprehensive resource skillfully consolidates crystal engineering, the design of organic solids, and supramolecular synthons (i.e., structural hydrogen bond units) to achieve desired pharmaceutical properties, including solubility, dissolution, bioavailability, permeability, particle size, tableting, hydration, and mechanical strength. Covering 30 years of crystal engineering developments and pharmaceutical applications, this book will be a single and complete resource for supramolecular and structural chemists, the crystal engineering community, pharmaceutical scientists, and industrial researchers. Key Features Covers the fundamentals of crystal engineering and supramolecular synthons. Details the challenges of low solubility and low permeability facing oral drug formulations. Explains how heterosynthons provide a rational approach to address and implement solutions. Provides case studies from academic and industrial labs to walk the reader through the actual steps. Explores developments in the scale up and manufacture of crystal forms in pharmaceutical industry.

Solid-State Properties of Pharmaceutical Materials
Solid-State Properties of Pharmaceutical Materials

Author: Stephen R. Byrn

Publisher: John Wiley & Sons

Published: 2017-07-12

Total Pages: 432

ISBN-13: 1119264448

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Presents a detailed discussion of important solid-state properties, methods, and applications of solid-state analysis Illustrates the various phases or forms that solids can assume and discussesvarious issues related to the relative stability of solid forms and tendencies to undergo transformation Covers key methods of solid state analysis including X-ray powder diffraction, thermal analysis, microscopy, spectroscopy, and solid state NMR Reviews critical physical attributes of pharmaceutical materials, mainly related to drug substances, including particle size/surface area, hygroscopicity, mechanical properties, solubility, and physical and chemical stability Showcases the application of solid state material science in rational selection of drug solid forms, analysis of various solid forms within drug substance and the drug product, and pharmaceutical product development Introduces appropriate manufacturing and control procedures using Quality by Design, and other strategies that lead to safe and effective products with a minimum of resources and time